Oligonucleotides containing 5-fluorouracil

Abstract

A homo-oligonucleotide of between 2 and 26 monomers of 5-fluorouridine 5'-monophosphate or 5-fluorodeoxyuridine 5'-monophosphate covalently linked via 3'- to 5'-phosphodiester linkages, where at the 3'- or 5'- terminus there is covalently linked a molecule selected from the group consisting of cholesterol, ethyl-spaced adamatane, 1,2-di-hexadecylglycerol and poly-L-lysine. These homo-oligonucleotides exhibit antitumor activity.

We claim: 
     
       1. A homo-oligonucleotide consisting essentially of between 2 and 26 monomers of 5-fluorodeoxyuridine 5'-monophosphate (FdUMP) covalently linked via 3'- to 5'-phosphodiester linkages, where at the 3'- or 5'-terminus there is covalently linked a molecule selected from the group consisting of cholesterol, ethyl-spaced adamatane, 1,2-di-hexadecylglycerol and poly-L-lysine. 
     
     
       2. The homo-oligonucleotide of claim 1 wherein said molecule is covalently linked only at the 3'-terminus. 
     
     
       3. The homo-oligonucleotide of claim 1 wherein said molecule is covalently linked only at the 5'-terminus. 
     
     
       4. A homo-oligonucleotide consisting essentially of between 2 and 26 monomers of 5-fluorouridine 5'-monophosphate (FUMP) covalently linked via 3'- to 5'-phosphodiester linkages, where at the 3'- or 5'-terminus there is covalently linked a molecule selected from the group consisting of cholesterol, ethyl-spaced adamatane, 1,2-dihexadecylglycerol and poly-L-lysine. 
     
     
       5. The homo-oligonucleotide of claim 4 wherein said molecule is covalently linked only at the 3'-terminus. 
     
     
       6. The homo-oligonucleotide of claim 4 wherein said molecule is covalently linked only at the 5'-terminus. 
     
     
       7. A homo-oligonucleotide consisting essentially of between 2 and 26 monomers of 5-fluorodeoxyuridine 5'-monophosphate (FdUMP) covalently linked via 3'- to 5'-phosphothioate linkages, where at the 3'- or 5'-terminus there is covalently linked a molecule selected from the group consisting of cholesterol, ethyl-spaced adamatane, 1,2-di-hexadecylglycerol and poly-L-lysine. 
     
     
       8. The homo-oligonucleotide of claim 7 wherein said molecule is covalently linked only at the 3'-terminus. 
     
     
       9. The homo-oligonucleotide of claim 7 wherein said molecule is covalently linked only at the 5'-terminus. 
     
     
       10. A homo-oligonucleotide consisting essentially of between 2 and 26 monomers of 5-fluorouridine 5'-monophosphate (FUMP) covalently linked via 3'- to 5'-phosphothioate linkages, where at the 3'- or 5'-terminus there is covalently linked a molecule selected from the group consisting of cholesterol, ethyl-spaced adamatane, 1,2-dihexadecylglycerol and poly-L-lysine. 
     
     
       11. The homo-oligonucleotide of claim 10 wherein said molecule is covalently linked only at the 3'-terminus. 
     
     
       12. The homo-oligonucleotide of claim 10 wherein said molecule is covalently linked only at the 5'-terminus.